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Everolimus (Afinitor)

Raw research findings for this medication. Mostly single studies, not curated or confirmed robust.

About Everolimus

What it is

Everolimus is an mTOR inhibitor, a close relative of sirolimus: it blocks mTOR, a protein that controls cell growth, division and blood vessel formation. At higher doses it is a targeted cancer medicine for advanced breast, kidney and neuroendocrine cancers and for tumours in tuberous sclerosis; at lower doses it prevents rejection after kidney and liver transplants. It is sold as Afinitor and Zortress, among other names.

How genes come into it

Everolimus is broken down mainly by CYP3A4, with help from CYP3A5 and CYP2C8, and pumped out of cells by ABCB1. Studies have looked at these genes for its blood levels in transplant patients, and at genes of the mTOR pathway (MTOR, RPTOR, PIK3R1) for response and side effects in cancer. The findings come from single or a few studies, and there is no CPIC or DPWG guideline.

What research found

Every published finding on gene variants and Everolimus. Upload your DNA file to see which of these rows apply to you.

Rated evidence (8 rated variants)

PharmGKB weighs all studies of a variant and rates how strong the evidence is, from 1A (strongest) to 4.

CYP3A5 CYP3A5*1, CYP3A5*3: Level 3. Metabolism/PK: Breast Neoplasms, Heart transplantation, Kidney Neoplasms, Kidney Transplantation, Lung transplantation, Neuroendocrine Tumors. 6.

PIK3R1 rs10515074: Level 3. Toxicity: Breast Neoplasms, Hyperglycemia, Leukopenia. 1.

MTOR rs2024627: Level 3. Efficacy: Breast Neoplasms, Kidney Neoplasms, Neuroendocrine Tumors. 1.

FGFR4 rs351855: Level 3. Efficacy: Discontinuation. 1.

Metabolism (14 findings)

Studies of how quickly the body processes this medication.

CYP3A4 rs35599367: Genotype AG is associated with increased concentrations of everolimus in women with Breast Neoplasms as compared to genotype GG.

CYP3A5 rs776746: Genotypes CC + CT is associated with decreased clearance of everolimus in people with heart transplantation as compared to genotype TT.

CYP3A5 rs776746: Genotype CT is associated with decreased trough concentration of everolimus in people with Breast Neoplasms, Kidney Neoplasms or Neuroendocrine Tumors as compared to genotype CC.

ABCB1 rs1045642: Genotypes AG + GG are not associated with concentrations of everolimus in women with Breast Neoplasms as compared to genotype AA.

Dosing (1 finding)

Studies of how much of the drug people needed or tolerated.

CYP2C8 CYP2C8*1, CYP2C8*3: CYP2C8 *1/*1 is not associated with dose of everolimus in people with heart transplantation as compared to CYP2C8 *1/*3.

Study findings and evidence levels: PharmGKB (CC BY-SA 4.0). Guidelines: CPIC and DPWG, as bundled in PharmCAT. Most studies were done mainly in people of European ancestry.

Related Drugs

More drugs from the same category

Torisel (mTOR Inhibitors)

Rapamune (mTOR Inhibitors)

5-FU (Antimetabolites)

Not a prescribing recommendation. This page is educational information about pharmacogenomic research and clinical guidelines - it is not medical or dosing advice, and not a prediction of how any medication will work for you. Never start, stop, or change a medication or dose based on it; talk to your doctor or pharmacist, who can order clinical-grade testing if appropriate.

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Content updated September 2026.

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